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Process for synthesis of prulifloxacin and its pharmaceutical composition

A composition and drug technology, applied in antibacterial drugs, organic chemistry, etc., can solve the problems of complex process, high cost, long route, etc., and achieve the effects of high yield, easy operation, and simple design

Inactive Publication Date: 2005-12-07
哈尔滨健迪医药技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The existing synthetic methods are complex in process, long in route and high in cost

Method used

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  • Process for synthesis of prulifloxacin and its pharmaceutical composition
  • Process for synthesis of prulifloxacin and its pharmaceutical composition
  • Process for synthesis of prulifloxacin and its pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] (II-a) (R is ethyl) (200g), tert-butanol (3500mL), potassium hydroxide (300g) in aqueous solution (1000mL), mix, reflux for 3 hours, filter and add ice water 5000mL, wash with concentrated hydrochloric acid Adjust the pH to 7, filter, wash with water, and dry to obtain light yellow solid (II) (150g).

[0028] TLC: Chloroform: Methanol = 1:1 (2 drops of ammonia) R f =0.3

Embodiment 2

[0030] (IV) (X is Br) (205g), dimethylformamide (2000mL), under ice water cooling, dropwise add dimethylformamide (500mL) of anhydrous piperazine (86g), after adding, continue Stir for 5 minutes to obtain compound (III).

Embodiment 3

[0032] Add (IV) (265g) and potassium bicarbonate (160g) to the mixture of (III), raise the temperature to room temperature, react for 6 hours, filter, the reaction solution is washed into ice water (10L), filter, and dry to obtain plulisa Star Crude (240g). The yield is 90.6%, the content is 98.5%, the moisture is 0.6%, the loss on drying is 13.0%, and the residue on ignition is 0.1%.

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Abstract

The invention discloses a novel process for preparing (+-)-6-fluoro-1-methyl-7-[4-(5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl-1-piperazinyl]-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid, and medicinal compositions containing the compound, which can be used for treating bacterial infection for mammals, and especially has strong effect in resisting Gram-negative bacteria.

Description

technical field [0001] The present invention relates to prulifloxacin ((±)-6-fluoro-1-methyl-7-[4-(5-methyl-2-oxo-1,3-dioxol-4 base) Methyl-1-piperazine]-4-oxo-4hydro-[1,3]thiazetidino[3,2-α]quinoline-3-carboxylic acid) (I) new synthetic antibacterial drug synthesis process. [0002] [0003] (I) technical background [0004] Synthetic antibacterial agents widely used in the treatment of infections caused by Gram-negative bacteria include enoxacin, ofloxacin, and ciprofloxacin. However, these antibacterial preparations cannot meet the growing and refractory diseases in recent years, namely the treatment of chronic Pseudomonas aeruginosa infection and Gram-negative bacterial infection. It has good absorption, excellent pharmacokinetic properties, broad antibacterial spectrum and strong antibacterial effect, and is a clinically effective antibacterial preparation. [0005] The antibacterial preparation was the first to be a new generation of a...

Claims

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Application Information

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IPC IPC(8): C07D513/04
Inventor 彭海生徐静
Owner 哈尔滨健迪医药技术有限公司
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